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ivabradine
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- ivabradine is a 'heart rate-reducing' agent able to slow heart rate, without
complicating side-effects (1)
- action results from a selective and specific block of pacemaker f-channels
of the cardiac sinoatrial node (SAN) - investigation has shown that block
by ivabradine requires
- open f-channels
- is use dependent
- is affected by the direction of current flow
- selective for the If current
- ivabradine lowers heart rate at concentrations that does not affect
other cardiac ionic currents
- ivabradine blocks If channels in a concentration-dependent manner
by entering the channel pore from the intracellular side
- blockade is only possible when the If channel is open
- magnitude of If inhibition is directly related to the frequency of channel opening
- unlike other heart rate-lowering mechanisms, direct If blockade
depends on the current driving force, as block dramatically
increases across the voltage interval, and on sodium concentration
in the surrounding milieu
- ivabradine would be expected to be most effective at higher heart rates, where its clinical usefulness would also be greatest
- blockade is only possible when the If channel is open
- ivabradine blocks If channels in a concentration-dependent manner
by entering the channel pore from the intracellular side
- ivabradine lowers heart rate at concentrations that does not affect
other cardiac ionic currents
- specific heart-rate lowering with ivabradine reduces myocardial oxygen demand, simultaneously improving oxygen supply
- ivabradine has no negative inotropic or lusitropic effects, thus preserving ventricular contractility - also it does not change any major electrophysiological parameters unrelated to heart rate
- has superior anti-anginal and anti-ischaemic activity to placebo and is non-inferior to atenolol and amlodipine
- action results from a selective and specific block of pacemaker f-channels
of the cardiac sinoatrial node (SAN) - investigation has shown that block
by ivabradine requires
NICE have stated with respect to the use of ivabradine in heart failure:
- ivabradine is recommended as an option for treating chronic heart failure
for people:
- with New York Heart Association (NYHA) class II to IV stable chronic
heart failure with systolic dysfunction and
- who are in sinus rhythm with a heart rate of 75 beats per minute
(bpm) or more and
- who are given ivabradine in combination with standard therapy including
betablocker therapy, angiotensin-converting enzyme (ACE) inhibitors
and aldosterone antagonists, or when beta-blocker therapy is contraindicated
or not tolerated and
- with a left ventricular ejection fraction of 35% or less
- should only be initiated after a stabilisation period of 4 weeks on
optimised standard therapy with ACE inhibitors, beta-blockers and aldosterone
antagonists
- should be initiated by a heart failure specialist with access to a multidisciplinary heart failure team. Dose titration and monitoring should be carried out by a heart failure specialist, or in primary care by either a GP with a special interest in heart failure or a heart failure specialist nurse.
- with New York Heart Association (NYHA) class II to IV stable chronic
heart failure with systolic dysfunction and
The summary of product characteristics must be consulted before prescribing this drug.
Reference:
- Bucchi A et al. Properties of ivabradine-induced block of HCN1 and HCN4 pacemaker channels. J Physiol. 2006 Apr 15;572(Pt 2):335-46.
- NICE (November 2012).Ivabradine for treating chronic heart failure.
Last reviewed 01/2018
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